Abstract
A series of aryl semicarbazones containing a methylene bridge in their skeleton were synthesized as anticonvulsant agents. The strategy of introducing a methylene bridge was to increase the flexibility of the structures because of sp3 hybridization. Pharmacological evaluations of the compounds were performed by determination of their effects on pentylenetetrazole-induced seizure parameters and neurotoxicity in mice. The statistical analysis indicated that most of the synthesized compounds showed significant anticonvulsant activity in comparison with the control group. No remarkable neurotoxicity was observed in rotorod test. A QSAR study was performed using multiple linear regressions. The results of the QSAR study confirmed that the compounds with Br at para position of these new derivatives are more potent than para-ethoxy series.
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Acknowledgments
This study was supported by grants from Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences and Kerman Neuroscience Research Center, Kerman University of Medical Sciences. We thank Ms. Marjan Jalili Baleh and Ali Kazemi for their technical assistance.
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Mozaffari, S., Ghasemi, S., Baher, H. et al. Synthesis and evaluation of some novel methylene-bridged aryl semicarbazones as potential anticonvulsant agents. Med Chem Res 21, 3797–3808 (2012). https://doi.org/10.1007/s00044-011-9924-6
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DOI: https://doi.org/10.1007/s00044-011-9924-6